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. 2008 Nov 13;51(21):7005-9.
doi: 10.1021/jm800537a. Epub 2008 Oct 9.

Potential nicotinic acetylcholine receptor ligands from 2,4-methanoproline derivatives

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Potential nicotinic acetylcholine receptor ligands from 2,4-methanoproline derivatives

Anup B Patel et al. J Med Chem. .

Abstract

Potential nicotinic acetylcholine receptor (nAChR) ligands have been synthesized in which a methylisoxazole substituent is attached to the 1-position ( 26) of the 2-azabicyclo[2.1.1]hexane ring system or separated by "spacer" atoms ( 21 and 23). With ABT-594 as a model, a range of pyridine heterocycles have been attached to the 1-position via a -CH 2O- spacer ( 11, 14, and 6). The biological evaluation of target compounds showed there was no binding affinity at the alpha4beta2 and alpha3beta4 nAChR subtypes.

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